US9657023B2ActiveUtilityA1

Polymorph of Syk inhibitors

88
Assignee: GILEAD CONNECTICUT INCPriority: Jul 30, 2013Filed: Jul 29, 2014Granted: May 23, 2017
Est. expiryJul 30, 2033(~7.1 yrs left)· nominal 20-yr term from priority
A61P 35/00A61P 35/02A61P 37/00A61P 37/06A61P 25/02A61P 29/00A61P 25/00A61P 11/06A61P 19/02C07D 487/04C07C 309/04
88
PatentIndex Score
12
Cited by
163
References
9
Claims

Abstract

Polymorphs of a bis-mesylate salt of a compound of Formula I: or a hydrate thereof, are provided. The bis-mesylate salt may also be depicted as a compound of Formula IA: Provided herein are also compositions thereof, methods for their preparation and methods for such polymorphs.

Claims

exact text as granted — not AI-modified
What is claimed is: 
     
       1. Polymorph Form 3 of a monohydrate bis-mesylate salt of a compound of Formula I 
       
         
           
           
               
               
           
         
       
     
     
       2. A pharmaceutical composition comprising:
 Form 3 of a mononhydrate bis-mesylate salt of a compound of formula I: 
 
       
         
           
           
               
               
           
         
         and a pharmaceutical carrier, excipient, adjuvant, or vehicle. 
       
     
     
       3. The pharmaceutical composition of  claim 2 , wherein the bis-mesylate salt is a monohydrate, bis-mesylate salt polymorph characterized by;
 an X-ray diffraction pattern comprising 2θ-reflections, plus or minus 0.2 degrees 2θ, at 13.8, 16.9, 22.9, and 26.1; or 
 an X-ray diffraction pattern substantially as shown in  FIG. 1A or 1B . 
 
     
     
       4. The pharmaceutical composition of  claim 2 , wherein the bis-mesylate salt is a monohydrate, bis-mesylate salt polymorph characterized by:
 an X-ray diffraction pattern comprising 2θ-reflections, plus or minus 0.2 degrees 2θ, at 13.8, 16.9, 22.9, and 26.1. 
 
     
     
       5. The pharmaceutical composition of  claim 2 , wherein the bis-mesylate salt is a monohydrate, bis-mesylate salt polymorph characterized by an X-ray diffraction pattern substantially as shown in  FIG. 1A . 
     
     
       6. The pharmaceutical composition of  claim 2 , wherein the bis-mesylate salt is a monohydrate, bis-mesylate salt polymorph characterized by an X-ray diffraction pattern substantially as shown in  FIG. 1B . 
     
     
       7. The polymorph of  claim 1 , wherein said polymorph is characterized by an X-ray diffraction pattern comprising 2θ-reflections, plus or minus 0.2 degrees 2θ, at 13.8, 16.9, 22.9, and 26.1. 
     
     
       8. The polymorph of  claim 1 , wherein said polymorph is characterized by an Xray diffraction pattern substantially as shown in  FIG. 1A . 
     
     
       9. The polymorph of  claim 1 , wherein said polymorph is characterized by an X-ray diffraction pattern substantially as shown in  FIG. 1B .

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